Current development and study of new pesticides are focused on searching and discovery of pesticidal active compounds that not only have new structures but also have new targets. In the process of regulation and control of energy metabolism, conversion of pyruvic acid from glycolysis into acetyl CoA as substrate for tricarboxylic acid cycle is a very important stage. This conversion is catalyzed by pyruvic dehydrogenases. If the pyruvate dehydrogenases are inhibited, pyruvic acid would be reduced into lactic acid instead of being converted into acetyl CoA. Accordingly, the source of acetyl CoA required in tricarboxylic acid cycle is limited, resulting in reduced yield of Adenosine Triphosphate (ATP), resulting in energy metabolic disturbance and tissue blocking, and under serious conditions resulting in death. Based on this biochemical feature, the pyruvic dehydrogenase complex may be used as a target of pesticides. Currently, there are reports about inhibitors of pyruvic dehydrogenases. For example, thiamine pyrophosphate analogs A-1 and A-2 are reported as highly active inhibitors against pyruvic dehydrogenases in microbes.

Although the thiamine pyrophosphate analogs A are a group of highly active inhibitors against pyruvic dehydrogenases in microbes, these compounds are complex in structure, difficult in synthesis and have low value in application, especially have not yet shown application value in agriculture. Accordingly, with pyruvic dehydrogenases in microbes as target, novel highly active inhibitors are designed and synthesized by applicant of this invention. Specifically, novel structural compounds are discovered as microbicide useful in agriculture. Those novel compounds are significant and valuable in study and development of novel highly active microbicide.